Assay Detail
Binding
CHEMBL4351620
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Inhibition of biotinylated peptide binding to human GST-tagged PCAF bromodomain expressed in Escherichia coli Rosetta (DE3) measured after 15 hrs by HTRF assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.55 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4574669 | — | — | 1 | 8.15 |
| CHEMBL4543497 | — | — | 1 | 8.00 |
| CHEMBL4449143 | — | — | 1 | 7.85 |
| CHEMBL4439202 | — | — | 1 | 7.77 |
| CHEMBL4545594 | — | — | 1 | 7.66 |
| CHEMBL4453637 | — | — | 1 | 7.60 |
| CHEMBL4570924 | — | — | 1 | 7.52 |
| CHEMBL4527339 | — | — | 1 | 7.52 |
| CHEMBL4454700 | — | — | 1 | 7.50 |
| CHEMBL4454766 | — | — | 1 | 7.46 |
| CHEMBL4570969 | — | — | 1 | 7.44 |
| CHEMBL4471748 | — | — | 1 | 7.39 |
| CHEMBL4457684 | — | — | 1 | 7.33 |
| CHEMBL4565832 | — | — | 1 | 7.14 |
| CHEMBL4541223 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4574669 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4543497 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4449143 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4439202 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4545594 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4453637 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4570924 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4527339 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4454700 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4454766 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4570969 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4471748 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4457684 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4565832 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4541223 | — | IC50 | = | 125.0 | nM | 6.90 |